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In vitro/in vivo performance of different complexes of itraconazole used in the treatment of vaginal candidiasis BJPS
Mirza,Mohammad Aamir; Rahman,Mohammad Akhlaquer; Talegaonkar,Sushama; Iqbal,Zeenat.
A large majority of new chemical entities and many existing drug molecules exhibit poor aqueous solubility, which may limit their potential use in developing drug formulations, with optimum bioavailability. One of the approaches to improve the solubility of a poorly water soluble drug and eventually its bioavailability is complexation with agents like humic acid (HA), fulvic acid (FA), β-cyclodextrin (β-CD), 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and caffeine (Caff). The current work emphasized at employing these agents to prepare different complexes and their in vitro/in vivo assessment. All the complexes evaluated for their complexation efficiency and authenticated by molecular modeling; conformational analysis, differential scanning calorimetry (DSC),...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Itraconazole/complexes; Itraconazole/evaluation; Itraconazole/complexes; Itraconazole/in vitro; Itraconazole/in vivo performance; Vaginal candidiasis/treatment; Drugs/solubility; Drugs/formulation.
Ano: 2012 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502012000400020
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Biopharmaceutics classification system: importance and inclusion in biowaiver guidance BJPS
Arrunátegui,Lorena Barbosa; Silva-Barcellos,Neila Márcia; Bellavinha,Karime Rezende; Ev,Lisiane da Silveira; Souza,Jacqueline de.
Pharmacological therapy is essential in many diseases treatment and it is important that the medicine policy is intended to offering safe and effective treatment with affordable price to the population. One way to achieve this is through biowaiver, defined as the replacement of in vivo bioequivalence studies by in vitro studies. For biowaiver of new immediate release solid oral dosage forms, data such as intestinal permeability and solubility of the drug are required, as well as the product dissolution. The Biopharmaceutics Classification System (BCS) is a scientific scheme that divides drugs according to their solubility and permeability and has been used by various guides as a criterion for biowaiver. This paper evaluates biowaiver application,...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Medicines/biowaiver; Biopharmaceutics Classification System; Drugs/solubility; Drugs/permeability; Drugs/dissolution; Drugs/legislation.
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000100143
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Cyclodextrins and ternary complexes: technology to improve solubility of poorly soluble drugs BJPS
Miranda,Janisse Crestani de; Martins,Tércio Elyan Azevedo; Veiga,Francisco; Ferraz,Humberto Gomes.
Cyclodextrins (CDs) are cyclic oligosaccharides composed of D-glucopyranoside units linked by glycosidic bonds. Their main property is the ability to modify the physicochemical and biological characteristics of low-soluble drugs through the formation of drug:CD inclusion complexes. Inclusion complexation requires that host molecules fit completely or partially within the CD cavity. This adjustment is directly related to the physicochemical properties of the guest and host molecules, easy accommodation of guest molecules within the CD cavity, stoichiometry, therapeutic dose, and toxicity. However, dosage forms may achieve a high volume, depending on the amount of CD required. Thus, it is necessary to increase solubilization efficiency in order to use...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Cyclodextrins; Ternary complexes; Drugs/complexation; Water-soluble polymers/use; Drugs/solubility; Inclusion complexe.
Ano: 2011 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502011000400003
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Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification BJPS
Dezani,André Bersani; Pereira,Thaisa Marinho; Caffaro,Arthur Massabki; Reis,Juliana Mazza; Serra,Cristina Helena dos Reis.
Solubility and dissolution rate of drugs are of major importance in pre-formulation studies of pharmaceutical dosage forms. The solubility improvement allows the drugs to be potential biowaiver candidates and may be a good way to develop more dose-efficient formulations. Solubility behaviour of lamivudine, stavudine and zidovudine in individual solvents (under pH range of 1.2 to 7.5) was studied by equilibrium solubility and intrinsic dissolution methods. In solubility study by equilibrium method (shake-flask technique), known amounts of drug were added in each media until to reach saturation and the mixture was subjected to agitation of 150 rpm for 72 hours at 37 ºC. In intrinsic dissolution test, known amount of each drug was compressed in the matrix of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Drugs/solubility; Drugs/dissolution rate; Intrinsic dissolution/method; Intrinsic dissolution/biopharmaceutical classification; Biopharmaceutical Classification System.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000400026
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